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Modulation of Glucokinase Regulatory Protein: A Double-Edged Sword?

Trends in molecular medicine - 1 Oct 2015

Brouwers Martijn C G J, Jacobs Chantal, Bast Aalt, Stehouwer Coen D A, Schaper Nicolaas C

Abstract excerpt

The continuous search for drugs targeting type 2 diabetes mellitus (T2DM) has led to the identification of small molecules that disrupt the binding between glucokinase and glucokinase regulatory protein (GKRP). Although mice studies are encouraging, it will take years before these disruptors can be introduced to T2DM patients. Recently, genome-wide association studies (GWASs) have shown that variants in the gene...

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Identifiers

PMID: 26432016
DOI: 10.1016/j.molmed.2015.08.004

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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Modulation of Glucokinase Regulatory Protein: A Double-Edged Sword?PMID 26432016Read ↗

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Effects of coding variants in the glucokinase regulatory protein gene on hepatic glucose and triglyceride metabolism suggest a gene regulatory function of glucokinaseSemantic proximity Read ↗

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The GCKR-P446L gene variant predisposes to raised blood cholesterol and lower blood glucose in the P446L mouse-a model for GCKR rs1260326Semantic proximity Read ↗

Impaired GK-GKRP interaction rather than direct GK activation worsens lipid profiles and contributes to long-term complications: a Mendelian randomization study.Semantic proximity Read ↗

Functional glucokinase regulator gene variants have inverse effects on triglyceride and glucose levels, and decrease the risk of obesity in children.Semantic proximity Read ↗

Compromised chronic efficacy of a Glucokinase Activator AZD1656 in mouse models for common human <i>GCKR</i> variantsSemantic proximity Read ↗

Glucokinase activity suppresses hepatic cholesterol synthesis and triglyceride accumulation: A new model for the effects of the GKRP P466L common human variantSemantic proximity Read ↗

New-Generation Glucokinase Activators: Potential Game-Changers in Type 2 Diabetes TreatmentSemantic proximity Read ↗

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From clinicogenetic studies of maturity-onset diabetes of the young to unraveling complex mechanisms of glucokinase regulation.Semantic proximity Read ↗

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